Evaluation of carbazeran 4-oxidation and O6-benzylguanine 8-oxidation as catalytic markers of human aldehyde oxidase: impact of cytosolic contamination of liver microsomes was written by Xie, Jiarong;Saburulla, Nur Fazilah;Chen, Shiyan;Wong, Siew Ying;Yap, Ze Ping;Zhang, Linghua Harris;Lau, Aik Jiang. And the article was included in Drug Metabolism & Disposition in 2019.Reference of 1614-12-6 This article mentions the following:
We investigated contribution of microsomal CYP450, cytosolic AOX-1 to carbazeran 4-oxidation, O6-benzylguanine 8-oxidation in human liver microsomal, cytosolic, S9 fractions. Incubations containing carbazeran and human liver microsomes with or without exogenously added NADPH yielded comparable levels of 4-oxo-carbazeran. O6-Benzylguanine 8-oxidation occurred in microsomal incubations, and extent was increased by NADPH. Human recombinant CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4, CYP3A5 did not catalyze carbazeran 4-oxidation, whereas CYP1A2 was active in O6-benzylguanine 8-oxidation 1-1-Aminobenzotriazole, a pan-cytochrome P 450 inhibitor, decreased O6-benzylguanine 8-oxidation, but not carbazeran 4-oxidation, in microsomal incubations, whereas 1-aminobenzotriazole and furafylline did not inhibit carbazeran 4-oxidation or O6-benzylguanine 8-oxidation in human liver S9 fraction. Carbazeran 4-oxidation in incubations containing human liver microsomes was attributed to microsomal preparations contaminated with AOX-1, as suggested by liver microsomal experiments indicating decrease in carbazeran 4-oxidation by an AOX-1 inhibitor (hydralazine), and to detection of AOX-1 protein. Cytosolic contamination of liver microsomes was further demonstrated by formation of dehydroepiandrosterone sulfate in liver microsomal incubations containing dehydroepiandrosterone. Carbazeran 4-oxidation, O6-benzylguanine 8-oxidation are enzyme-selective catalytic markers of AOX-1, as shown in S9 fraction expressing cytochrome P 450 and AOX-1. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Reference of 1614-12-6).
1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. However, triazoles are also useful in bioorthogonal chemistry, because the large number of nitrogen atoms causes triazoles to react similar to azides. Both the triazoles and their derivatives have significant biological properties including antimicrobial, antiviral, antitubercular, anticancer, anticonvulsant, analgesic, antioxidant, anti-inflammatory, and antidepressant activities.Reference of 1614-12-6
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics